PF-04217903 is an orally bioavailabe, small-molecule MET tyrosine kinase inhibitor with potential antineoplastic activity.
PF-04217903 demonstrates exquisite kinase selectivity. Inhibition studies of the c-Met mutants show that PF-04217903 is more susceptible to oncogenic mutations that attenuate potency than PF-02341066.
PF-04217903 was evaluated against multiple kinase selectivity screening panels: Invitrogen Inc. (125 kinases), Millipore/Upstate Ltd. (105 kinases), University ofDundee (51 kinases), and Pfizer in-house (48 kinases) (Supporting Information). On the basis of the percent inhibition or IC50 values generated from each of these screens, PF-04217903 was estimated to be>1000-fold selective for c-Met compared with each of the other kinases included in these collective screening assays.